氟甲噻嗪 | 148-56-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 中文名称: 氟甲噻嗪
• 英文名称: 7-Sulfamoyl-6-trifluormethyl-1,2,4-benzothiadiazin-1,1-dioxid
• 英文别名: Flumethiazide；1,1-dioxo-6-(trifluoromethyl)-4H-1λ6,2,4-benzothiadiazine-7-sulfonamide
• CAS: 148-56-1
• 化学式: C₈H₆F₃N₃O₄S₂
• 分子量: 329.281
• InChiKey: RGUQWGXAYZNLMI-UHFFFAOYSA-N

物化性质

• 熔点：
  306.6°C
• 沸点：
  560.0±60.0 °C(Predicted)
• 密度：
  1.6578 (estimate)
• 颜色/状态：
  CRYSTALS
• 溶解度：
  0.15 M

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  135
• 氢给体数：
  2
• 氢受体数：
  9

ADMET

毒理性

• 相互作用

噻嗪类药物的管状运输可能会被丙磺舒抑制。/苯并噻二嗪类/

TUBULAR TRANSPORT OF THIAZIDES MAY BE INHIBITED BY PROBENECID. /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

肠溶衣组合使用氯化钾和噻嗪类药物与远端空肠或回肠溃疡高发病率有关。建议开具可口的氯化钾溶液处方... /BENZOTHIADIAZIDES/

USE OF ENTERIC-COATED COMBINATIONS OF POTASSIUM CHLORIDE & THIAZIDE HAS BEEN ASSOC WITH HIGH INCIDENCE OF ULCERATION OF DISTAL JEJUNUM OR ILEUM. IT IS PREFERABLE TO PRESCRIBE PALATABLE SOLN OF POTASSIUM CHLORIDE... /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

噻嗪类利尿剂与醛固酮拮抗剂或其他保钾利尿剂联合使用，以获得加性的利尿效果并维持钾平衡。/苄噻嗪类/

...THIAZIDE DIURETICS HAVE BEEN PRESCRIBED IN COMBINATION WITH ALDOSTERONE ANTAGONIST OR OTHER POTASSIUM-SPARING DIURETIC IN ORDER TO OBTAIN ADDITIVE DIURETIC EFFECT WITH MAINTENANCE OF POTASSIUM BALANCE. /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

临床毒性相对罕见，通常是由意外的超敏反应引起的。有报道称出现紫癜、具有光敏性的皮炎、血液形成成分的抑制以及坏死性血管炎的情况... /苄硫噻嗪类/

CLINICAL TOXICITY IS RELATIVELY RARE & USUALLY RESULTS FROM UNEXPECTED HYPERSENSITIVITY. CASES HAVE BEEN REPORTED WITH PURPURA, DERMATITIS WITH PHOTOSENSITIVITY, DEPRESSION OF FORMED ELEMENTS OF BLOOD, & NECROTIZING VASCULITIS... /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

血浆尿酸经常升高，在易感患者中可能与痛风发作有关。许多观察者已经注意到与低钾血症和碱中毒有关联。据报道，血氨浓度升高。/苯噻嗪类/

PLASMA URIC ACID IS FREQUENTLY ELEVATED & IN SUSCEPTIBLE PT MAY BE ASSOCIATED WITH ATTACKS OF GOUT. ... MANY OBSERVERS HAVE NOTED CORRELATION WITH HYPOKALEMIA & ALKALOSIS. INCR CONCN OF BLOOD AMMONIA HAVE BEEN REPORTED. /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

噻嗪类药物通过胃肠道吸收，它们的有用性主要归功于它们通过口服途径的有效性。吸收相对较快。...药物容易通过胎盘屏障传递给胎儿。...大多数化合物在3-6小时内迅速排泄。/苄噻嗪类/

THIAZIDES ARE ABSORBED FROM GASTROINTESTINAL TRACT & OWE THEIR USEFULNESS LARGELY TO THEIR EFFECTIVENESS BY ORAL ROUTE. ABSORPTION IS RELATIVELY RAPID. ... DRUG PASSES READILY THROUGH PLACENTAL BARRIER TO FETUS. ... MOST COMPD ARE RAPIDLY EXCRETED WITHIN 3-6 HR. /BENZOTHIADIAZIDES/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 海关编码：
  2935009090

反应信息

• 作为反应物：
  描述：

  氟甲噻嗪 在 氯磺酸 作用下， 生成 6-trifluoromethyl-7-chlorosulfonyl-1,2,4-benzothiadiazine-1,1-dioxide
  参考文献：
  名称：

  7-Mercapto(or thio)-benzothiadiazine products

  摘要：

  本文描述了7-巯基（或烷基或芳基硫）-1,2,4-苯并噻二嗪-1,1-二氧化物化合物。通过将7-氯磺酰取代基还原为7-巯基，然后，如果需要，烷基化或芳基化以提供7-硫取代基来制备产品。另外，可以通过已知的程序将4-RS-邻氨基苯酰胺环化以提供3-未取代或3-取代的类似物。产品是黄嘌呤氧化酶抑制剂。

  公开号：

  US03951967A1

文献信息

• NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
  申请人：Ryono Denis E.

  公开号：US20080009465A1

  公开（公告）日：2008-01-10

  Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R 4 is —(CH 2 ) n -Z-(CH 2 ) m —PO(OR 7 )(OR 8 ), —(CH 2 ) n Z-(CH 2 ) m —PO(OR 7 )R g , —(CH 2 ) n -Z-(CH 2 ) m —OPO(OR 7 )R g , —(CH 2 ) n Z—(CH 2 ) m —OPO(R 9 )(R 10 ), or —(CH 2 ) n Z—(CH 2 ) m —PO(R 9 )(R 10 ); R 5 and R 6 are independently selected from H, alkyl and halogen; Y is R 7 (CH 2 ) s or is absent; and X, n, Z, m, R 4 , R 5 , R 6 , R 7 , and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

  提供了磷酸酯和磷酸酯激活剂，因此在治疗糖尿病和相关疾病方面非常有用，并具有以下结构： 其中 是杂环芳基环； R 4 为—(CH 2 ) n -Z-(CH 2 ) m —PO(OR 7 )(OR 8 )、—(CH 2 ) n Z-(CH 2 ) m —PO(OR 7 )R g 、—(CH 2 ) n -Z-(CH 2 ) m —OPO(OR 7 )R g 、—(CH 2 ) n Z—(CH 2 ) m —OPO(R 9 )(R 10) 或—(CH 2 ) n Z—(CH 2 ) m —PO(R 9 )(R 10) ； R 5 和R 6 分别选择自H、烷基和卤素； Y为R 7 (CH 2 ) s 或不存在；以及 X、n、Z、m、R 4 、R 5 、R 6 、R 7 和s如本文所定义；或其药用盐。 还提供了一种利用上述化合物治疗糖尿病和相关疾病的方法。
• PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY
  申请人：Rewcastle Gordon William

  公开号：US20110009405A1

  公开（公告）日：2011-01-13

  Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.

  本文提供了式I的嘧啶基和1,3,5-三嗪基苯并咪唑化合物，以及它们的药物组合物、制备方法，以及作为抗癌治疗药物或药剂的用途，可以单独使用，也可以与放疗和/或其他抗癌药物联合使用。
• SUBSTITUTED INDOLES
  申请人：Gant Thomas G.

  公开号：US20090191183A1

  公开（公告）日：2009-07-30

  Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

  本文揭示了Formula I的替代吲哚半胱氨酸白三烯受体调节剂，其制备方法，药物组合物以及使用方法。
• (ALPHA-SUBSTITUTED ARALKYLAMINO AND HETEROARYLALKYLAMINO) PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE IN TREATING PROLIFERATIVE DISEASES
  申请人：Brown S. David

  公开号：US20120252802A1

  公开（公告）日：2012-10-04

  Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.

  本文提供了（α-取代的芳基氨基或杂环芳基氨基）嘧啶基和1,3,5-三嗪基苯并咪唑类化合物，例如，式I的化合物，以及它们的药物组合物、制备方法，以及作为治疗增殖性疾病的药剂或药物的用途。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
  申请人：Cerulean Pharma Inc.

  公开号：US20130196906A1

  公开（公告）日：2013-08-01

  Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.

  提供了关于使用CDP-治疗剂偶联物治疗疾病或紊乱的方法，例如自身免疫疾病、炎症性疾病、中枢神经系统紊乱、心血管疾病或代谢紊乱。还提供了CDP-治疗剂偶联物、包含CDP-治疗剂偶联物的颗粒以及包含CDP-治疗剂偶联物的组合物。